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Ex vivo delta opioid receptor autoradiography: CNS receptor occupancy of two novel compounds over their antihyperalgesic dose range.

Discovered as part of an effort to identify delta opioid (DOPr or DOR) agonist analgesics, JNJ-20788560 and JNJ-39204880 exhibited high DOR affinity, with K(i) values of 1.7 and 2.0nM, respectively, and were selective for DOR over the mu opioid receptor (MOPr or MOR), with 596- and 122-fold selectivity, respectively. Both compounds stimulated DOR but not MOR induced GTPgammaS binding and were effective antihyperalgesic agents in the complete Freund's adjuvant model of thermal hyperalgesia in the rat, with oral ED(50) values of 13.5 and 35mg/kg, corresponding to plasma levels of 1 and 9microM,

[Cholestatic liver diseases].

Primary biliary cirrhosis (PBC), autoimmune cholangitis (AIC = AMA-negative PBC) and primary sclerosing cholangitis (PSC) are autoimmune cholestatic liver diseases. Overlap syndromes combine characteristics of cholestatic liver diseases and autoimmune hepatitis. In PBC, alkaline phosphatase and gamma-glutamyl transferase are elevated, to a lesser degree aminotransferases. Histology shows bile duct lesions. Anti-mitochondrial antibodies are typical. Ursodeoxycholic acid (UDC) is established therapy that slows or even stops the disease progression, at least in early stages of the disease. In non

Pruritus in Systemic Diseases: A Review of Etiological Factors and New Treatment Modalities.

Pruritus is the most frequently described symptom in dermatology and can significantly impair the patient's quality of life. In 10-50% of adults with persistent pruritus, it can be an important dermatologic clue for the presence of a significant underlying systemic disease such as renal insufficiency, cholestasis, hematologic disorder, or malignancy (Etter and Myers, 2002; Zirwas and Seraly, 2001). This review describes the presence of pruritus in different systemic diseases. It is quite important to discover the cause of pruritus for providing relief for the patients experiencing substantial

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… Naltrexone, oral μ -opioid antagonist, showed dramatic response in the treatment of renal pruritus. Recently, nalfurafine (TRK-820), a kappa-receptor agonist, has also shown beneficial effects in the severe ESRD-associated pruritus. … Naltrexone has an oral-dosing route and so can be used as an effective antipruritic, especially in this kind of pruritus. The main side effects are nausea, vomiting, fatigue, and dizziness [ 46 ]. …

Presynaptic kappa-opioid and muscarinic receptors inhibit the calcium-dependent component of evoked glutamate release from striatal synaptosomes.

In addition to cytosolic efflux, reversal of excitatory amino acid (EAA) transporters evokes glutamate exocytosis from the striatum in vivo. Both kappa-opioid and muscarinic receptor agonists suppress this calcium-dependent response. These data led to the hypothesis that the calcium-independent efflux of striatal glutamate evoked by transporter reversal may activate a transsynaptic feedback loop that promotes glutamate exocytosis from thalamo- and/or corticostriatal terminals in vivo and that this activation is inhibited by presynaptic kappa and muscarinic receptors. Corollaries to this hypoth

Immunomodulatory action of class mu-, delta- and kappa-opioid receptor agonists in mice.

Endogenous opioids exert a variety of functions outwith the central nervous system, including modulation of some murine lymphocyte functions. The results of this study indicate that mu-, delta- and kappa-receptor selective agonists are potent in vitro stimulators of mitogen-induced proliferation of murine T-lymphocytes. Moreover, the observed enhancement of mitogen-induced proliferation was reversed by mu-, delta- and kappa-receptor class selective antagonists, beta-funaltrexamine, ICI 174,864 and nor-binaltorphimine, respectively. An additional study has revealed that repeated administration

The Protective Effects of Κ-Opioid Receptor Stimulation in Hypoxic Pulmonary Hypertension Involve Inhibition of Autophagy Through the AMPK-MTOR Pathway.

BACKGROUND/AIMS: In a previous study, we showed that κ-opioid receptor stimulation with the selective agonist U50,488H ameliorated hypoxic pulmonary hypertension (HPH). However, the roles that pulmonary arterial smooth muscle cell (PASMC) proliferation, apoptosis, and autophagy play in κ-opioid receptor-mediated protection against HPH are still unknown. The goal of the present study was to investigate the role of autophagy in U50,488H-induced HPH protection and the underlying mechanisms. METHODS: Rats were exposed to 10% oxygen for three weeks to induce HPH. After hypoxia, the mean pulmonary

Peripherally acting mu-opioid-receptor antagonists and the connection between postoperative ileus and pain management: The anesthesiologist's view and beyond.

The adverse effects of opioids are well documented. Because opioid receptors have a wide-ranging anatomic distribution, the effects subsequent to opioid binding, both good and bad, occur centrally and in the periphery. Postoperative strategies to reduce opioid burden, therefore, are in the patient's best interest. Multimodal analgesia is the key towards balancing the need for opioids while simultaneously reducing their burden. Alternative anesthesia and analgesia options such as regional anesthesia, nonsteroidal anti-inflammatory drugs, or cyclooxygenase-2 enzyme inhibitors should be considere

delta-Opioid receptor antagonists inhibit GIRK channel currents in acutely dissociated brainstem neurons of rat.

In this study, we investigated the effects of delta-opioid receptor antagonists on the G protein-coupled inwardly rectifying potassium (GIRK) channel currents induced by serotonin (5-HT) and noradrenaline (NAd) in the dorsal raphe and the locus coeruleus neurons, respectively. Perforated patch and conventional whole-cell patch clamp recording techniques were used for the study. Neurons were acutely dissociated from neonatal rats. Both naltrindole (NTI) and naltriben (NTB), which are selective delta-antagonists possessing antitussive activity in in vivo animal studies, reversibly inhibited the

Involvement of mesolimbic structures in short-term sodium depletion: in situ hybridization and ligand-binding analyses.

Acute treatment with the diuretic furosemide (Lasix) produces a reduction in plasma Na(+) and volume as well as increased thirst and salt appetite. The resulting hypovolemia stimulates the well-known counter-regulatory physiological response from the renin-angiotensin-aldosterone system. However, the neurochemical players underpinning the behavioral responses of thirst and salt appetite are less clear. Previously, we have reported that salt-replete deoxycorticosterone (DOCA) treatment activates mesolimbic structures associated with reward and goal-seeking behavior. The present study was design

Neuroprotective agents in acute ischemic stroke.

The concept of neuroprotection relies on the principle that delayed neuronal injury occurs after ischemia. The phenomenon of the "ischemic cascade" has been described, and each step along this cascade provides a target for therapeutic intervention. A wide variety of drugs have been studied in humans. Ten classes of neuroprotective agents have reached phase III efficacy trials but have shown mixed results. They included calcium channel antagonists, NMDA receptor antagonists, lubeluzole, CDP-choline, the free radical scavenger tirilazad and ebselen, enlimomab, GABA agonist clomethiazole, the sod

Role of central mu-opioid receptors in the modulation of nitric oxide production by splenocytes.

Previous studies have shown that administration of morphine results in alterations of splenic macrophage nitric oxide production. The presen … k syndrome toxin (TSST-1). The effect of DAMGO is blocked by prior i.c.v. administration of N-methylnaltrexone. In contrast, i.c.v. administration of the kappa-selective agonist, U69,593, and the delta-selective agonist, DPDPE, have no significant effect on the production of nitric oxide. Furthermore, the in vitro administration of DAMGO, DPDPE, or U69,593 t …

Both T cells and macrophages are targets of kappa-opioid-induced immunosuppression.

We have previously shown that antibody responses are inhibited following administration of kappa-opioid agonists. We found that the inhibition was blocked by either naloxone or the kappa-selective antagonist norbinaltorphimine. This inhibitory activity is apparent after short-term treatment with the kappa-opioid agonist. In an attempt to identify the cell populations which serve as the target for this immunosuppressive effect, we have carried out cell fractionation analyses to generate isolated T cells and macrophages. Using multiple cell fractionation methods, we have determined that short-te

Idiopathic osteoporosis, Ehlers-Danlos syndrome, postural orthostatic tachycardia syndrome, and mast cell activation disorder in a 27-year-old male patient: A unique case presentation.

A young male patient presents with widespread pain and varying chronic inflammatory symptoms for three years and idiopathic low bone density for more than ten years. Based on the patient's clinical history, the patient has been diagnosed with an hypermobile Ehlers-Danlos syndrome, postural orthostatic tachycardia syndrome, and mast cell activation disorder trifecta with affiliated inflammation-induced osteoporosis.

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… Moreover, while not a documented or proven therapeutic regimen, therapy was started with daily 6.0 mcg low‐dose naltrexone (LDN) due to its positive pain‐relieving effects in patients with chronic pain disorders and its role as a toll‐like receptor (TLR4) antagonist 6 in addition to 20 mcg H1 antihistamines … Low‐dose naltrexone (LDN)‐review of therapeutic utilization . Med Sci (Basel) . 2018 ; 6 ( 4 ): 82 . doi: 10.3390/medsci6040082 PMC6313374 30248938 7 “ HEDS Diagnostic Checklist .” Diagnostic Criteria for Hypermobile Ehlers‐Danlos Syndrome (hEDS), Version 9. …

Drug treatment of obesity.

Both diet and medications are useful in the treatment of the obese patient. Weight loss of about 10% below baseline can be achieved with both, and there is no evidence that the composition of the diet, by itself, has any influence on weight loss. Presently only 1 drug is approved for long-term treatment of overweight patients, and its effectiveness is limited to palliation of the chronic disease of obesity. Combinations of medications and antidiabetic drugs that produce weight loss are being evaluated.

Prodynorphin-derived peptides are critical modulators of anxiety and regulate neurochemistry and corticosterone.

Stress and anxiety are mainly regulated by amygdala and hypothalamic circuitries involving several neurotransmitter systems and providing physiological responses to peripheral organs via the hypothalamic-pituitary-adrenal axis and other pathways. The role of endogenous opioid peptides in this process is largely unknown. Here we show for the first time that anxiolytic parameters of explorative behavior in mice lacking prodynorphin were increased 2-4-fold in the open field, the elevated plus maze and the light-dark test. Consistent with this, treatment of wild-type mice with selective kappa-opio

Noradrenaline is necessary for the hedonic properties of addictive drugs.

To determine whether noradrenaline (NA) is an essential neurotransmitter for addictive and appetitive behaviors, we measured drug and food seeking in transgenic mice lacking dopamine beta-hydroxylase (Dbh), the enzyme responsible for synthesizing NA. Using the conditioned place preference test (CPP), we show that Dbh -/- mice do not exhibit rewarding behavior to morphine, cocaine, or the mixed reuptake inhibitor bupropion. In spite of their lack of preference for drugs, Dbh -/- mice had an unaltered preference for food. Drug seeking was induced when NA was restored to the central nervous syste

Clinical Practice Guidelines for management of Sexual Disorders in Elderly.

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… Other drugs: Naltrexone, an opiate antagonist, can antagonize the inhibition of sexual functions. Aswagandha, Shathavari, Korean red ginseng are helpful in enhancing sexual functioning in both males and females. Aswagandha (Indian ginseng) enhances sexual desire in men. … TherClin Risk Manag 2014 10 341 354 Published online 2014 May 14. doi: 10.2147/TCRM.S39727 10.2147/TCRM.S39727 PMC4027935 24868160 63 Van Ahlen H Piechota H.J Kias H.J Brennemann W Klingmuller D Opiate antagonistsin erectile dysfunction: a possible new treatmentoption Results of a pilot study with Naltrexone …

Сексуальная диагностика после травматологического травматизма мозга и разрушения мозга: критический нарационный обзор нейробиологии, клинических фенотипов и управления.

Фон/цели: Приобретенная травма мозга (АБИ) может нарушить сексуальное регулирование, но в литературе не поддерживается ни одна связь между побочными повреждениями. В этом критическом обзоре дается оценка гиперсексуальности, сексуального лишения и редких парафических проявлений после травматической травмы мозга (ТБР) и инсульта, а также задается вопрос о том, насколько скудные, разнородные данные могут служить основой для пропорционального клинического ухода. Методы: была проведена проверка по Пубмеду/МЕДЛИНЕ, Скопу и Сети наук 6 Август 2026. Two Эксперты, проводящие обзор, проводят независимую

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… The remaining publications are the sertraline-associated hypomania report [ 31 ] and two non-ABI naltrexone treatment reports [ 32 , 33 ]; their comparator roles are explicit in Supplementary Tables S2 and S3 . … Sources: [ 15 , 166 , 167 , 171 , 172 , 173 , 174 , 175 ] Naltrexone Possible specialist option for selected reward-driven or compulsive patterns. No direct post-ABI evidence identified. Level 4 indirect evidence from non-ABI case reports. …

PROTOCOL: Opioid-specific medication-assisted therapy and its impact on criminal justice and overdose outcomes.

BACKGROUND: The overlap between criminal justice system involvement and drug use is well-documented, and criminal justice agencies have been … tudies had to prospectively test the effects of heroin and methadone maintenance, buprenorphine, or naltrexone on criminal conviction, arrest, revocation of community supervision, technical probation or parole violation, mandated treatment failure, and specialized court docket failure. Overdose outcomes were also examined for samples in criminal justice sett …

Inhibition of urinary bladder motility by a spinal action of U-50488H in rats.

We examined the effect of a kappa agonist, U-50488H, upon the bladder motility of anaesthetized rats. The frequency of distension-induced rhythmic bladder contractions was reduced by the intravenous (10 mg kg(-1)) or intrathecal (10-100 microg) administration of U-50488H. The effect of intravenous U-50488H was inhibited by pre-treatment with nor-binaltorphimine (10 mg kg(-1), s.c.). The inhibition of bladder contractions by intrathecal U-50488H (30 microg) was eliminated with the concomitant use of nor-binaltorphimine (10 mg kg(-1), s.c.), and diminished by reserpine (4 mg kg(-1), i.p.), yohim